Tetrahydroquinoline derivatives as opioid receptor antagonists.
Article Details
- CitationCopy to clipboard
Zhang C, Westaway SM, Speake JD, Bishop MJ, Goetz AS, Carballo LH, Hu M, Epperly AH
Tetrahydroquinoline derivatives as opioid receptor antagonists.
Bioorg Med Chem Lett. 2011 Jan 15;21(2):670-6. doi: 10.1016/j.bmcl.2010.12.010. Epub 2010 Dec 8.
- PubMed ID
- 21193310 [ View in PubMed]
- Abstract
Opioid receptors play an important role in both behavioral and homeostatic functions. We herein report tetrahydroquinoline derivatives as opioid receptor antagonists. SAR studies led to the identification of the potent antagonist 2v, endowed with 1.58nM (K(i)) functional activity against the mu opioid receptor. DMPK data suggest that novel tetrahydroquinoline analogs may be advantageous in peripheral applications.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Naltrexone Kappa-type opioid receptor Ki (nM) 10 N/A N/A Details Naltrexone Mu-type opioid receptor Ki (nM) 2 N/A N/A Details